DRUGS etc.

NOTE: Before turning to sleep aids to improve your sleep problems, it may be more useful to take a look at your sleep hygiene to eliminate any bad habits which may affect your ability to fall asleep or to maintain sleep.

If your sleep hygiene is impeccable and you still struggle with sleep, you might be experiencing drug interactions or side effects from treating other health conditions.

The more substances you take, even if they are nutritional supplements or over the counter, the more likely you are going to run into interactions and unexpected side effects.

That said, sometimes a pharmaceutical treatment is the best option for your particular sleep disorder.

Whatever you choose, please have this open conversation with your doctor first. Remember, they can advise you not only with regard to drug therapies, but to non-drug techniques as well.

With all this in mind… What are the most commonly used substances and how do they impact sleep?

Common Substances

Caffeine

We know coffee, tea, cola, energy drinks, and chocolate are commonly known to rev up the brain. Caffeine decreases sleepiness and will shorten total sleep duration, reduce deep sleep, and increase the chance for arousals.

Withdrawal from caffeine creates an increase in daytime sleepiness, headaches that could interfere with sleep, and an increase in deep nonREM sleep. Reliance on caffeine can actually contribute to further daytime sleepiness because it can interfere with quality sleep at night and leave you sleep deprived.

Cigarettes

Smoking provides a double whammy when it comes to affecting sleep. Nicotine is a stimulant, though it may trick smokers into thinking that it relaxes them.

Nicotine addiction can lead to fragmented sleep as it arouses some sleepers to get up and smoke in the middle of the night; this can lead to insomnia, fragmented sleep, and a reduction in deep sleep. For this reason, smoking right before bed practically guarantees you will experience poor sleep.

Over the long term, smoking leads to many breathing disorders, such as Chronic Obstructive Pulmonary Disease (COPD), a combination of emphysema and chronic bronchitis which can significantly impair one’s ability to maintain an adequate oxygen supply in the bloodstream at night, leading to dangerous issues like hypoxemia.

Alcohol

It may seem like the perfect sleep aid, but the nightly nightcap is not doing you any favors.

It can also amplify negative mood issues, which can affect one’s ability to fall asleep.

Withdrawal from marijuana use can also lead to several days of poor sleep until the drug is fully metabolized from the bloodstream. Even the withdrawal that occurs after a bedtime “toke” may account for periods of sleeplessness in the middle of the night, which is similar to alcohol withdrawal.

Over-the-counter Drugs

Nonprescription pain relievers

What could be wrong with taking pain relievers at bedtime? It seems like they should be a first-line defense against insomnia related to chronic pain.

Pain can be one of the worst enemies of sleep; a person who is in chronic pain may never be able to settle in comfortably in order to sleep. However, some pain relievers can disrupt sleep patterns.

Several popular over-the-counter options, like Excedrin, Motrin Complete, and Anacin, can contain caffeine, which can last up to eight hours in the bloodstream. It’s always a best practice to read the labels on your over-the-counter drugs; if they have caffeine in them, it will show up on the label.

Over-the-counter (OTC) sleep aids: do they work?

Maybe. Maybe not.

Some OTC sleep aids work more as a matter of belief (as in “the placebo effect.”)

Others work due to the science behind their ingredients. Most OTC sleep aids contain some form of antihistamine, which may or may not be helpful and which may or may not have side effects or drug interactions.

Most prescription sleeping pills will help you fall asleep, though not everybody responds to them in the same way. They also have a host of side effects to consider:

Drug dependence or habituation

“Morning after” hangover

Cognitive dysfunction

Dry mouth

Some sleep aids are also not meant to be used nightly over the long term. An occasional dose is okay, but over weeks and months, other serious problems can develop which may require discontinuation.

Beyond the most common sedative hypnotics listed above are the following other classes of drugs that may be prescribed to help with sleep (or wakefulness).

Anti-anxiety medications (anxiolytics)

These shorten the time it takes to fall asleep, help you to stay asleep at night, and can help you feel refreshed when you wake up. However, sleep architecture changes with the use of these drugs: you get more light sleep, but your deep sleep stages will be reduced, perhaps significantly.

You can develop a tolerance to these drugs which, should you decide to stop taking them, can have a temporary impact on your sleep patterns until you have gone through withdrawal. Anti-anxiety drugs (aka “downers”) include benzodiazepines (“benzos” or “bennies”); barbiturates (“barbies”); drugs with a chloral hydrate component; and the sedative hypnotics listed above.

Stimulant drugs

By their very definition, stimulants are not indicated for good sleep in general. They shorten the amount of sleep you get, reduce your deep sleep, make it harder to fall asleep, and break up sleep into fragments.

However, stimulants or “wakefulness promoting drugs” are sometimes prescribed for people who are severely sleepy during the day.

Stimulant drugs (“uppers”) include any form of amphetamine and dopaminergic drugs (drugs which enhance dopamine response in the brain), which include, commonly, pramipexole, clozapine, Ritalin, modafinil, and Wellbutrin.

Antidepressant medications

These drugs are known to have a major impact on sleep. They can either significantly increase or decrease the quality and quantity of sleep you get. Generally speaking, they all commonly reduce the amount of REM sleep you get, sometimes eliminating this important stage altogether.

Antidepressants are broken into several categories: Tricyclics, MAOIs, SSRIs, and SNRIs.

Antipsychotic medications

These medications used for schizophrenic patients tend to normalize fragmented sleep, leading to increased sleepiness and more deep sleep. However, users of antipsychotics have a high potential for insomnia upon withdrawal of use of these drugs.

Other Prescriptions (not for sleep)

Below, you’ll find the most common prescription drugs NOT TYPICALLY PRESCRIBED AS SLEEP AIDS which can still have a negative impact on your sleep health or ability to stay awake during the day.

Your best best for determining how your particular prescriptions influence your sleep habits is to consult with your pharmacist and/or physician. They can research interactions and consider the side effects together,with all of your other therapies, to best determine if your sleep problems are coming from your medications or from other physical conditions you may have.

This list is by no means exhaustive. Keep in mind that if single medications can impact sleep, so too can combined medications. Drug interactions can be problematic when it comes to sleep.

Vitamins and/or supplements

Don’t be tricked into believing you can escape side effects of drugs by using vitamins and nutritional supplements to treat your sleep issues.

While there is some evidence that you can improve your sleep quality through nutraceuticals, some supplements—including vitamins and herbs—can have a negative impact on your ability to sleep. Listed below are a few to consider.

Common vitamins and minerals and their impact on sleep

Calcium helps to stimulate melatonin production in the brain, so it can be useful as a sleep aid. Melatonin is a natural substance secreted by the pineal gland in the late afternoon which regulates the sleep/wake cycle; its main role is encouraging sleep at night as part of your circadian rhythm.

Folic acid deficiency may be a trigger for nightly insomnia.

Iron deficiency is a common cause of Restless Leg Syndrome (RLS), which can be a problem as well at night. Another condition, Periodic Leg Movement Disorder, is similar to RLS in that the legs constantly twitch or are difficult to relax once someone has fallen asleep. Often, an iron supplement can be the simple solution to this annoying problem.

Magnesium is well known as a relaxation mineral and can also help to alleviate nocturnal leg cramps.

Vitamins B6 and B12 are both known for generating vivid dream states. This can lead to sleep disruption night after night, so you may wish to take these supplements in the morning. On the other hand, B6 also has a calmative effect, so if you are not bothered by active REM sleep and need something to help you relax, B6 might be the right fit for you.

Vitamin D seems to improve symptoms of excessive daytime sleepiness in some people, though the mechanisms to explain this are not understood.

Vitamin E, like iron, can help to alleviate problems with daytime and nighttime restless legs.

Zinc offers many of magnesium’s same relaxing properties.

Nutritional supplements and their impact on sleep

5-HTP (5-Hydroxytryptophan), derivative of the amino acid L-tryptophan, is often safely taken as a sleep aid, as it causes drowsiness.

Copper as a supplement is very stimulating and a cause of insomnia for many.

GABA is an amino acid produced by the brain which naturally aids in calming the brain; there are synthetic and natural supplements available, but the jury is still out on whether these can positively improve the sleeping process.

Glutathione has a double edge: oxidized forms of glutathione (GSSH) can improve deep sleep, but a lack of naturally occurring glutathione in the body can cause insomnia.

The amino acids L-phenylalanine, S-adenosyl-L-methionine, and L-tyrosine have stimulating effects which can lead to trouble sleeping at night.

Melatonin is the darling of the nutraceutical world; the exogenous (synthetic) form is taken to help enhance the brain’s own ability to generate its own endogenous (naturally occurring) melatonin via the pineal gland. Melatonin levels are critical to the chemistry of the human circadian system and should be higher during dim light and nighttime than during the day. Therefore, timing of melatonin dosage is critical to its effectiveness.

L-theanine is also believed to support relaxation and sleep at night.

Herbs and their impact on sleep

Camellia sinensis is a kind of green tea which is thought to increase the brain’s natural theanine levels, which support good sleep.

Chamomile tea is famously known to relax the mind in preparation for sleep.

Guarana is a highly concentrated form of caffeine and, therefore, not a friend to sleep, but good for people who are excessively sleepy.

Korean Ginseng may disturb your sleep and cause insomnia, but it is also know for shortening sleep onset because of its stress relieving properties.

Skullcap is a plant whose upper foliage is used to treat insomnia.

St. John’s Wort is another commonly used herb for sleep disorders; it can help you sleep more soundly, contains exogenous melatonin, and supports the brain’s own melatonin manufacture.

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THE SHC MISSION

The SleepyHeadCENTRAL mission is to develop an accessible, accurate, and user-friendly online clearinghouse of sleep information.

This effort is designed to help educate healthcare consumers on the vital importance of sleep in overall optimal health.

My aim as Curator is to give healthcare consumers clear and empowering options to actively address their sleep problems.

---Tamara Sellman RPSGT CCSH, Curator

ABOUT THE CURATOR

Tamara Kaye Sellman is a registered polysomnographic technologist (RPSGT) and certified clinical sleep health educator (CCSH). She is also a sleep apnea patient and lives with hypersomnia partly caused by multiple sclerosis.

Sellman holds a degree in journalism from Columbia Chicago ('90) and is an independent sleep health journalist.

She currently serves as an independent journalist and blogger working for industry associations. She also generates educational materials for the American Association of Sleep Technologists, writes a weekly column for their blog, and contributes to their educational and content strategy committees. She served as Secretary of the Washington State Sleep Society between 2013-2018.

Among her other journalism efforts are award-winning contributions to publications of the American Association of Sleep Technologists (A2Zzz and the AAST blog).

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The SleepyHeadCENTRAL website and related newsletter and all other publications are not intended to substitute for medical advice. If you or a loved one has problems with sleeping (or not sleeping), please consult your doctor immediately. || HIPAA regulations do not permit the release of private health information of any kind on this website/ newsletter. Any letters directed to the SHC mailbox will be considered anonymously for publication and, as necessary, revised to protect the identity of those making inquiries. || SHC has not received compensation of any kind in exchange for any giveaway services or products or comments, blog posts, opinions or other communications which mention any giveaway services or products. || Product or service reviews and their links in this newsletter are posted as opinion and are not considered formal product or service endorsements. || Unsolicited queries by marketing agents and freelance writers will be deleted unread; multiple attempts will be reported as spam and/or blocked. Guest posts are by invitation only and are limited to board-certified healthcare professionals with whom we have a previous relationship.